In clinics, the liver fibrosis staging often depends on liver biopsy and Metavir classification which is classified F0, F1, F2, F3 and F4 according to the biopsy observation under microscopy. The biggest challenge for this method was its abhorrence by people for its latent danger. Besides, it is not accurate due to the frequent sampling error and deviation of individual observation. Furthermore, the result is qualitative and subjective but not quantitative and objective.
It has been well documented by Lee laboratory since 1983 that multivalent galactopeptide has a strong “cluster effect” to enhance binding with hepatic Gal/GalNAc receptor. The Gal-terminated triantennary structure exhibits 106 fold stronger affinities than monovalent component structure. After binding, the galactopeptide will be endocytosis into hepatic cell. In 2004, Kwon's experiment indicates that the ischemic hepatic membrane has much lower Gal/GalNAc receptor and meanwhile, the endocytosis is also much less than the normal liver cell.
This invention discloses a molecular imaging method for quantification of liver fibrosis grade and its glyco-imaging agent with liver-targeting characteristics. This liver targeting glyco-molecular imaging provides the exact image distribution and real hepatic cellular uptake value, which objectivity overcomes the numerous uncertainty of present method.